^3H—去甲乌药碱的合成

Synthesis of 3 H-higenamine

目的 合成3H 去甲乌药碱。方法 以 1 (4 甲氧基苄基 ) 6 ,7 二甲氧基 3,4 二氢 异喹啉为前体 ,采用催化氚气加成反应及氢溴酸脱甲氧基反应合成3H 去甲乌药碱。标记物经薄层层析纯化 ,经紫外分光光度法 (UV)和高效液相色谱法 (HPLC)进行质量鉴定。结果 合成的3H 去甲乌药碱UV和HPLC图谱鉴定与去甲乌药碱标准品一致 ,放化纯 >98% ,比活度 >370GBq mmol。结论 该微量合成3H 去甲乌药碱的方法为去甲乌药碱的药代动力学研究提供了物质基础。

Objective To synthesize 3 H higenamine. Methods The synthesis consisted of catalytic tritium gas addition and demethoxylation. 3 H higenamine was purified by thin layer chromatography and identified by UV and HPLC. Results The UV and HPLC spectrum of the synthesized 3 H higenamine were identical with that of the higenamine standard, the radiochemical purity was more than 98% and the specific activity was 370 GBq/mmol. Conclusion An effective method for synthesis of 3 H higenamine in small scale is developed, and it makes the further pharmacodynamical research of higenamine feasible.